Drug intelligence / Profile preview

isorhapontigenin

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral
01

Overview

Isorhapontigenin is a naturally occurring tetrahydroxylated stilbenoid with a methoxy group, structurally related to resveratrol and an isomer of rhapontigenin. It is found in several plants, including the Chinese herbs Gnetum cleistostachyum and Gnetum parvifolium, as well as the seeds of Aiphanes aculeata. Isorhapontigenin exhibits multiple biological activities such as anti-inflammatory, antineoplastic (anti-cancer), cardioprotective, antiviral, and antioxidant effects[1][2][3]. Mechanistically, it has been shown to induce autophagy and cell death in cancer cells via caspase-dependent pathways; inhibit sphingosine kinases (SPHK1/2), leading to tubulin destabilization; suppress pro-inflammatory cytokines (TNF-α, IL-6, IL-1β); inhibit MAPK/PI3K signaling; regulate cell cycle arrest; modulate Sirt1 activity; protect cardiac microvasculature by inhibiting ferroptosis through PRDX2-MFN2-ACSL4 pathways[4][5][7][8]. Its highest development status for any indication appears to be preclinical research for lung cancer[10].

Other names
isorhapontigeninisorhapotogenin
02

Targets

P2Y12 (Purinergic P2Y12 receptor)

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